Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds

…, PD Dans, FJ Luque, S Conde, A Martínez

文献索引：Conde, Santiago; Perez, Daniel I.; Martinez, Ana; Perez, Concepcion; Moreno, Francisco J. Journal of Medicinal Chemistry, 2003 , vol. 46, # 22 p. 4631 - 4633

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被引用次数: 39

摘要

Development of kinase-targeted therapies for central nervous system (CNS) diseases is a great challenge. Glycogen synthase kinase 3 (GSK-3) offers a great potential for severe CNS unmet diseases, being one of the inhibitors on clinical trials for different tauopathies. Following our hypothesis based on the enhanced reactivity of residue Cys199 in the binding site of GSK-3, we examine here the suitability of phenylhalomethylketones as irreversible ...